Catalog No.S1548 Synonyms: BMS-512148
Molecular Weight(MW): 408.87
Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.
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(B) Clonogenic survival of prostate cancer cells treated with Canagliflozin, Dapagliflozin or Salicylate and expressed relative to the vehicle controls.
Mol Metab, 2016, 5(10):1048-56.. Dapagliflozin purchased from Selleck.
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|Description||Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.|
|Features||More potent stimulator of glucosuria than other SGLT2 inhibitors.|
Dapagliflozin is not sensitive to hSGLT1 with a 1200-fold IC50.  Dapagliflozin is 32-fold more potent than phlorizin against hSGLT2 but 4-fold less than phlorizin against hSGLT1. Dapagliflozin is highly selective versus GLUT transporters and displays 8–9% inhibition in protein-free buffer at 20 μM and virtually no inhibition in the presence of 4% bovine serum albumin.  Dapagliflozin has good permeability across Caco-2 cell membranes and is a substrate for P-glycoprotein (P-gp) but not a significant P-gp inhibitor. Dapagliflozin is stable in rat, dog, monkey, and human serum at 10 μM. Dapagliflozin shows no inhibitory responses or induction to human P450 enzymes. The in vitro metabolic pathways Dapagliflozin are glucuronidation, hydroxylation, and O-deethylation. 
|In vivo||Dapagliflozin reduces blood glucose levels by 55% after 0.1 mg/kg oral dose in hyperglycemic streptozotocin (STZ) rats, which is in part to the metabolic stability conferred by the C-glucoside linkage. Dapagliflozin displays a favorable absorption, distribution, metabolism, and excretion (ADME) profile and is orally bioavailable.  Dapagliflozin (1 mg/kg) causes significant dose-dependent glucosuria and increase in urine volume in normal rats over 24 hours post-dose. Dapagliflozin induces increase in urine glucose and urine volume excretion at 6 hours post-dose in Zucker diabetic fatty (ZDF) rats. Dapagliflozin lowers fasting and fed glucose levels in ZDF rats even by 2 weeks of treatment, without any marker of renal or liver toxicity.  Dapagliflozin significantly reduces the development of hyperglycaemia, with lowered blood glucose. Dapagliflozin could improve the insulin sensitivity, reduce β-cell mass and the development of impaired pancreatic function. |
|In vitro||DMSO||82 mg/mL (200.55 mM)|
|Ethanol||17 mg/mL (41.57 mM)|
|In vivo||30% PEG400+0.5% Tween80+5% propylene glycol||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03036150||Recruiting||Chronic Kidney Disease||AstraZeneca||February 2017||Phase 3|
|NCT03036124||Not yet recruiting||Chronic Heart Failure With Reduced Ejection Fraction (HFrEF)||AstraZeneca||February 2017||Phase 3|
|NCT02987738||Not yet recruiting||Type1diabetes||Kinderkrankenhaus auf der Bult|AstraZeneca|Alcedis GmbH||February 2017||Phase 1|
|NCT03030235||Not yet recruiting||Chronic Heart Failure With Preserved Systolic Function||Saint Lukes Health System||February 2017||Phase 4|
|NCT02919345||Not yet recruiting||Diabetes Mellitus, Type 2|Coronary Artery Disease|Carotid Artery Diseases||University of Campinas, Brazil|AstraZeneca||January 2017||Phase 4|
|NCT02981966||Not yet recruiting||Diabetes Mellitus, Type 2||The University of Texas Health Science Center at San Antonio|AstraZeneca||January 2017||Phase 4|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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